[HTML][HTML] The prostaglandin D2 receptor 2 pathway in asthma: a key player in airway inflammation

C Domingo, O Palomares, DA Sandham… - Respiratory …, 2018 - Springer
Asthma is characterised by chronic airway inflammation, airway obstruction and hyper-responsiveness.
The inflammatory cascade in asthma comprises a complex interplay of genetic …

Fevipiprant (QAW039), a slowly dissociating CRTh2 antagonist with the potential for improved clinical efficacy

…, A Miah, C Bauer, SJ Watson, DA Sandham… - Molecular …, 2016 - ASPET
Here we describe the pharmacologic properties of a series of clinically relevant chemoattractant
receptor-homologous molecules expressed on T-helper type 2 (CRTh2) receptor …

Discovery of icenticaftor (QBW251), a cystic fibrosis transmembrane conductance regulator potentiator with clinical efficacy in cystic fibrosis and chronic obstructive …

…, P Wright, A Young, DA Sandham - Journal of Medicinal …, 2021 - ACS Publications
Mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel
are established as the primary causative factor in the devastating lung disease cystic fibrosis (…

7-Azaindole-3-acetic acid derivatives: Potent and selective CRTh2 receptor antagonists

DA Sandham, C Adcock, K Bala, L Barker… - Bioorganic & medicinal …, 2009 - Elsevier
High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2
receptor antagonist chemotype, which could be optimised to furnish a highly selective …

Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma

DA Sandham, L Barker, L Brown, Z Brown… - ACS Medicinal …, 2017 - ACS Publications
Further optimization of an initial DP 2 receptor antagonist clinical candidate NVP-QAV680
led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl…

Uncoupling the structure–activity relationships of β2 adrenergic receptor ligands from membrane binding

…, DJJ McKay, J Reilly, DA Sandham… - Journal of medicinal …, 2016 - ACS Publications
Ligand binding to membrane proteins may be significantly influenced by the interaction of
ligands with the membrane. In particular, the microscopic ligand concentration within the …

A convergent synthesis of the renin inhibitor CGP60536B

DA Sandham, RJ Taylor, JS Carey, A Fässler - Tetrahedron Letters, 2000 - Elsevier
Pseudoephedrine serves as a dual purpose chiral auxiliary and protecting group in the
synthesis of the novel orally active renin inhibitor CGP60536B.

An investigation into the structure–activity relationships associated with the systematic modification of the β2-adrenoceptor agonist indacaterol

…, D Janus, EM Rosethorne, DA Sandham… - Bioorganic & medicinal …, 2012 - Elsevier
The synthesis of a series of indacaterol analogues in which each of the three structural regions
of indacaterol are modified in a systematic manner is described. Evaluation of the affinity …

[HTML][HTML] The roles of type 2 cytotoxic t cells in inflammation, tissue remodeling, and prostaglandin (pg) d2 production are attenuated by pgd2 receptor 2 antagonism

…, ID Pavord, P Klenerman, DA Sandham… - The Journal of …, 2021 - journals.aai.org
Human type 2 cytotoxic T (Tc2) cells are enriched in severe eosinophilic asthma and can
contribute to airway eosinophilia. PGD 2 and its receptor PGD 2 receptor 2 (DP2) play …

Fevipiprant, a selective prostaglandin D2 receptor 2 antagonist, inhibits human group 2 innate lymphoid cell aggregation and function

…, ID Pavord, VJ Erpenbeck, DA Sandham… - Journal of Allergy and …, 2019 - jacionline.org
We thank Drs Daniel Rotrosen and Alkis Togias from the National Institute of Allergy and
Infectious Diseases for their review of the manuscript, Ms Monica Campbell from the University …